Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold

X He, L Wang, Z Zheng, J Xiao, W Zhong…

Index: He, Xinhua; Wang, Lili; Zheng, Zhibing; Xiao, Junhai; Zhong, Wu; Li, Song Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 1 p. 553 - 557

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Abstract

A series of oxazolidin-2-one-4-carboxylic amide compounds (1a–f) were designed and synthesized as the non-phosphate S1P1 receptor agonists. The single crystal of 1e was prepared and solved to elucidate the structure of 1a–f. EC50 of 1a–d were about 1.1–3.6 μM in S1P1 Redistribution® assay, and their cytotoxicity was 8–40-fold lower than FTY720. Though its S1P1 agonist activities in vitro were about 1000-folds weaker than (S)-FTY720- ...

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